Protein Degradation & Proteostasis

VH032

CAS 1448188-62-2

VH-032 (VHL ligand 1) is a VHL ligand for PROTAC and potent, small molecule inhibitor of the VHL/HIF-1α interaction with Kd of 185 nM.

UC-764865

CAS 2566480-63-3

UC-764865 (UC764865) is a small-molecule inhibitor that targeted ubiquitin-conjugating enzyme UBE2N active site.UC-764865 blocks ubiquitination of innate immune- and inflammatory-related substrates in human AML cell lines.Inhibition of UBE2N function…

Cyclosporin A

CAS 59865-13-3

Cyclosporin A is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM.

Thalidomide

CAS 50-35-1

Thalidomide can directly inhibit angiogenesis induced by bFGF or VEGF in vivo.Thalidomide was commonly used therapeutically in the late 1950's; however, it was withdrawn from the market when it was discovered to cause birth defects. More recent research has…

ARV-102

CAS 3080678-93-6

ARV-102 is a highly potent, orally bioavailable PROTAC that targets LRRK2 with a of 0.14 nM, designed to cross the blood-brain barrier to address neurodegenerative diseases. By hijacking the body’s ubiquitin-proteasome system, it achieves deep and sustained…

4μ8C

CAS 14003-96-4

4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.

IXA6

CAS 1021106-40-0

IXA6 is a novel small molecule compound of inducing IRE1 RNase activity.

IXA4

CAS 1185329-96-7

IXA4 is the most selective for the IRE1–XBP1s signaling pathway.IXA4 selectively activate IRE1–XBP1s signaling and reduces secretion of APP through IRE1 activation.

BAY-8040 (R)

CAS 1194453-23-0

Bay-8040 is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 28 nM; displays no significant inhibition toward 68 other pharmacologically relevant targets (>10 uM), and a panel of related serine proteases; shows in vivo efficacy with…

S-methyl-KE-298

CAS 143584-75-2

S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.

QC-01–175

CAS 2267290-96-8

QC-01-175 is a hetero-bifunctional molecule designed to engage both tau and Cereblon (CRBN) to trigger tau ubiquitination and proteasomal degradation (tau PROTAC).QC-01–175 effected clearance of tau in frontotemporal dementia (FTD) patient-derived neuronal…

SB405483

SB-405483 is a specific small-molecule chemical compound used in scientific research as an allosteric ligand for the protein cereblon (CRBN). It is primarily a biochemical tool for studying protein degradation pathways and has potential implications for drug…

6-TG/Thioguanine

CAS 154-42-7

6-Thioguanine is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2,…

HB007

CAS 2387821-46-5

HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers[1][2].

MS4078

CAS 2229036-62-6

MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 19 nM for binding affinity to ALK[1].

BC1618

CAS 2222094-18-8

BC1618 is a novel Fbxo48 inhibitor and prevent pAmpkα degradation with MEC (minimal efficacious concentration) of 0.6 μM.

MS177

CAS 2225938-86-1

MS177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.MS177 effectively degraded cellular EZH2-PRC2, suppressed global H3K27me3 in leukaemia cells.MS177…

Usp22i-S02

CAS 309735-96-4

Usp22i-S02(USP22-IN-1, compound S02) is a potent inhibitor of ubiquitin specific peptidase 22 (USP22). It showed anticancer activity by suppressing Foxp3 expression in T-regulatory cells.

E3 Ligand-Linker Conjugate 8

CAS 1957235-74-3

An E3 ligase ligand-linker conjugate for PROTAC.

Foldamer 33

CAS 1651890-48-0

Foldamer 33 is a small molecule HSP110 inhibitor, directly binds to the nucleotide-binding domain (NBD) of HSP110, blocks HSP110 chaperone function and colorectal cancer growth.Foldamer 33 significantly inhibit HSP110 anti-aggregating activity with IC50 of…

Autotaxin-IN-8

CAS 2756388-01-7

BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78. BSJ-05-037 induces potent degradation of ITK dependent on CRBN, neddylation, and the proteasome. BSJ-05-037 induces GATA-3 loss…

RS-0406

CAS 530112-00-6

RS-0406 is a novel beta-sheet breaker, RS-0406 reverses amyloid beta-induced cytotoxicity and impairment of long-term potentiation in vitro. RS-0406 arrests amyloid-beta oligomer-induced behavioural deterioration in vivo.

Tri-GalNAc-PEG8-Gly-Gly-Gly(Tri-GalNAc-G3)

Tri-GaNAc-PEG8-Gly-Gly-Gly is a compound that targets the asialoglycoprotein receptor (ASGPR) and is utilized to conjutate with antibody.

Tri-GalNAc-PEG8-NH2-CH2CH2-NH2-bromoacetyl (Tri-GalNAc-Haloacetyls)

Tri-GaNAc-PEG8-NH2-CH2CH2-NH2-bromoacetyl is a compound that targets the asialoglycoprotein receptor (ASGPR) and is utilized to conjutate with antibody.

HDAC3 PROTAC P7

HDAC3 PROTAC P7 is a potent and selective HDAC3-directed PROTAC with IC50 of 40 nM (HDAC3 deacetylase activity), effectively induces HDAC3 degradation with DC50 of 0.6 nM in THP-1 cells (Emax=90%).

E3 ligase Ligand 1A ((S,R,S)-AHPC-Me)

CAS 1948273-02-6

E3 ligase Ligand 1A is a ligand of E3 ligase, used in PROTAC technology; E3 ligase Ligand 1A can be used in the research of cancer.

VHL ligand 2 hydrochloride ((S,R,S)-AHPC-Me hydrochloride)

CAS 1948273-03-7

VHL ligand 2 hydrochloride is a Ligand for E3 Ligase extracted from patent WO/2017/030814A1 compound example 202, used in PROTAC technology.

MS.001

CAS 53619-67-3

MS.001 is a small molecule that inhibits both the chaperone binding and ubiquitin ligase activity of C-terminus of Hsc70 interacting protein (CHIP) at low micromolar concentrations (IC50=3.3 uM).

ARV-825

CAS 1818885-28-7

ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome.…